RU2006141835A - Tetra-Substituted Imidazole Derivatives as Modulators of CB1 Cannabinoid Receptors with High Selectivity for Subtypes of CB1 / CB2 Receptors - Google Patents

Tetra-Substituted Imidazole Derivatives as Modulators of CB1 Cannabinoid Receptors with High Selectivity for Subtypes of CB1 / CB2 Receptors Download PDF

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RU2006141835A
RU2006141835A RU2006141835/04A RU2006141835A RU2006141835A RU 2006141835 A RU2006141835 A RU 2006141835A RU 2006141835/04 A RU2006141835/04 A RU 2006141835/04A RU 2006141835 A RU2006141835 A RU 2006141835A RU 2006141835 A RU2006141835 A RU 2006141835A
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Йозефус Х. М. ЛАНГЕ (NL)
Йозефус Х. М. Ланге
Хендерик К. ВАЛС (NL)
Хендерик К. ВАЛС
Корнелис Г. КРУСЕ (NL)
Корнелис Г. Крусе
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Солвей Фармасьютикалс Б.В. (Nl)
Солвей Фармасьютикалс Б.В.
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Abstract

The present invention relates to 1,2,4,5-tetrasubstituted imidazole derivatives as selective cannabinoid CB1 receptor modulators, in particular CB1 receptor antagonists or inverse agonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said imidazole derivatives. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. A beneficial effect is disclosed herein or apparent to a person skilled in the art from the specification and general knowledge in the art. The invention also relates to the use of a compound of the invention for the manufacture of a medicament for treating or preventing a disease or condition. More particularly, the invention relates to a new use for the treatment of a disease or condition disclosed herein or apparent to a person skilled in the art from the specification and general knowledge in the art. In embodiments of the invention specific compounds disclosed herein are used for the manufacture of a medicament useful in the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.

Claims (12)

1. Соединение общей формулы (I),1. The compound of General formula (I),
Figure 00000001
(I)
Figure 00000001
(I) в которой R1 представляет собой атом хлора, брома, фтора или водорода,in which R 1 represents an atom of chlorine, bromine, fluorine or hydrogen, R2 представляет собой атом хлора или брома или группу CF3,R 2 represents a chlorine or bromine atom or a CF 3 group, А представляет собой атом азота или группу СН,A represents a nitrogen atom or a CH group, Х представляет собой атом серы или сульфоксидную (S=O) группу, или сульфоновую (SO2) группу,X represents a sulfur atom or a sulfoxide (S = O) group, or a sulfonic (SO 2 ) group, Y представляет собой атом водорода или метильную, этильную, н-пропильную, изопропильную, н-бутильную, трет-бутильную, трифторметильную, фенильную, бензильную или пиридильную группу,Y represents a hydrogen atom or a methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, trifluoromethyl, phenyl, benzyl or pyridyl group, Z представляет собой атом азота или группу СН,Z represents a nitrogen atom or a CH group, n представляет собой число 1, 2 или 3,n represents the number 1, 2 or 3, и таутомеры, стереоизомеры и фармакологически приемлемые соли соединений.and tautomers, stereoisomers and pharmacologically acceptable salts of the compounds. 2. Соединения по п.1 общей формулы (I), в которой R1 представляет собой атом водорода или атом хлора, R2 представляет собой атом хлора, Y представляет собой метильную или этильную группу, Z представляет собой СН, n обозначает 1, 2 или 3, А и Х имеют значения как в п.1, и таутомеры, стереоизомеры и фармакологически приемлемые соли соединений.2. The compounds according to claim 1 of general formula (I), in which R 1 represents a hydrogen atom or a chlorine atom, R 2 represents a chlorine atom, Y represents a methyl or ethyl group, Z represents CH, n represents 1, 2 or 3, A and X are as defined in claim 1, and the tautomers, stereoisomers and pharmacologically acceptable salts of the compounds. 3. Соединение по п.2 общей формулы (I), в которой R1 представляет собой атом хлора, Y представляет собой метильную группу, А представляет собой атом азота, и таутомеры, стереоизомеры и фармакологически приемлемые соли соединений.3. The compound according to claim 2 of general formula (I), in which R 1 represents a chlorine atom, Y represents a methyl group, A represents a nitrogen atom, and tautomers, stereoisomers and pharmacologically acceptable salts of the compounds. 4. Фармацевтические композиции, включающие в себя фармакологически активное количество по меньшей мере одного соединения по пп.1-3 или соль такого соединения в качестве активного ингредиента, а также фармацевтически приемлемый носитель и/или по меньшей мере одно фармацевтически приемлемое вспомогательное вещество.4. Pharmaceutical compositions comprising a pharmacologically active amount of at least one compound according to claims 1-3, or a salt of such a compound as an active ingredient, as well as a pharmaceutically acceptable carrier and / or at least one pharmaceutically acceptable excipient. 5. Способ получения фармацевтических композиций по п.4, отличающийся тем, что по меньшей мере одно соединение по пп.1-3 объединяют с фармацевтически приемлемым носителем и/или вспомогательным веществом и таким образом переводят в форму, подходящую для введения.5. A method for producing pharmaceutical compositions according to claim 4, characterized in that at least one compound according to claims 1 to 3 is combined with a pharmaceutically acceptable carrier and / or excipient and thus is converted into a form suitable for administration. 6. Соединение по любому из пп.1-3 или его соль в качестве активного ингредиента лекарственного средства.6. The compound according to any one of claims 1 to 3 or its salt as the active ingredient of the drug. 7. Соединение общей формулы (IV),7. The compound of General formula (IV),
Figure 00000002
(IV)
Figure 00000002
(Iv) в которой Y представляет собой метильную, этильную, н-пропильную, изопропильную, н-бутильную, трет-бутильную, трифторметильную, фенильную, бензильную или пиридильную группу, и R1, R2, X и Z имеют значения, указанные в п.1.in which Y represents a methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, trifluoromethyl, phenyl, benzyl or pyridyl group, and R 1 , R 2 , X and Z have the meanings specified in paragraph 1 . 8. Соединения общей формулы (V),8. The compounds of General formula (V),
Figure 00000003
(V)
Figure 00000003
(V) в которой Y представляет собой метильную, этильную, н-пропильную, изопропильную, н-бутильную, трет-бутильную, трифторметильную, фенильную, бензильную или пиридильную группу, и R1, R2, X и Z имеют значения, указанные в п.1.in which Y represents a methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, trifluoromethyl, phenyl, benzyl or pyridyl group, and R 1 , R 2 , X and Z have the meanings specified in paragraph 1 . 9. Применение соединения по любому из пп.1-3 для получения фармацевтической композиции для лечения психоза, чувства тревоги, депрессии, дефицита внимания, расстройства памяти, нарушений познавательной способности, нарушений аппетита, ожирения, в особенности юношеского ожирения и ожирения, вызванного лекарственными средствами, наркомании, влечения (например, полового), лекарственной зависимости и неврологических расстройств, таких, как нейродегенеративные нарушения, слабоумие, дистония, мышечная спастичность, тремор, эпилепсия, рассеянный склероз, травматическое повреждение головного мозга, удар, болезнь Паркинсона, болезнь Альцгеймера, эпилепсия, болезнь Гентингтона, синдром Туретта, церебральная ишемия, апоплексия мозга, черепно-мозговая травма, инсульт, повреждение позвоночника, нейровоспалительные нарушения, склеротические бляшки, вирусный энцефалит, нарушения, связанные с демиелинизацией, а также для лечения нарушений, связанных с болью, включая нарушения, связанные с нейропатической болью, и других заболеваний, связанных с каннабиноидной нейротрансмиссией, в том числе для лечения септического шока, глаукомы, рака, диабета, рвоты, тошноты, астмы, респираторных заболеваний, желудочно-кишечных расстройств, язвы желудка, диареи, половых нарушений и сердечно-сосудистых нарушений.9. The use of a compound according to any one of claims 1 to 3 for the preparation of a pharmaceutical composition for the treatment of psychosis, anxiety, depression, attention deficit disorder, memory impairment, cognitive impairment, appetite disturbances, obesity, especially juvenile obesity and drug-induced obesity , addiction, craving (e.g., sexual), drug dependence and neurological disorders such as neurodegenerative disorders, dementia, dystonia, muscle spasticity, tremor, epilepsy, are dispersed sclerosis, traumatic brain damage, stroke, Parkinson’s disease, Alzheimer's disease, epilepsy, Huntington’s disease, Tourette’s syndrome, cerebral ischemia, brain apoplexy, traumatic brain injury, stroke, spinal injury, neuro-inflammatory disorders, sclerotic plaques, viral encephalitis associated with demyelination, as well as for the treatment of disorders associated with pain, including disorders associated with neuropathic pain, and other diseases associated with cannabinoid neurotransmission, including including for the treatment of septic shock, glaucoma, cancer, diabetes, vomiting, nausea, asthma, respiratory diseases, gastrointestinal upsets, stomach ulcers, diarrhea, genital disorders and cardiovascular disorders. 10. Применение по п.9 соединения по любому из пп.1-3 для получения фармацевтической композиции для лечения нарушений аппетита, в особенности ожирения, юношеского ожирения и ожирения, индуцированного лекарственным средством.10. The use according to claim 9 of a compound according to any one of claims 1 to 3 for the preparation of a pharmaceutical composition for the treatment of appetite disorders, especially obesity, juvenile obesity and drug-induced obesity. 11. Применение по п.10. соединения по любому из пп.1-3 для получения фармацевтической композиции для лечения нарушений, связанных с питанием, в особенности ожирения, юношеского ожирения и ожирения, индуцированного лекарственным средством, отличающееся тем, что указанная фармацевтическая композиция содержит также по меньшей мере один ингибитор липазы.11. The use of claim 10. compounds according to any one of claims 1 to 3 to obtain a pharmaceutical composition for the treatment of disorders related to nutrition, in particular obesity, adolescent obesity and drug-induced obesity, characterized in that the pharmaceutical composition also contains at least one lipase inhibitor. 12. Применение по п.11, отличающееся тем, что указанный ингибитор липазы представляет собой орлистат или липстатин.12. The use according to claim 11, characterized in that said lipase inhibitor is orlistat or lipstatin.
RU2006141835/04A 2004-05-28 2005-05-26 Tetrasubstituted imidazole derivatives as cannabinoid cb1 receptor modulators, highly selective to subrange receptors cb1/cb2 RU2354650C2 (en)

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